Key result
[14C]JP-1366 was rapidly absorbed and extensively metabolized, with 94.3% of the administered radioactive dose recovered through excretion, predominantly via feces and urine.
Why the study?
To characterize the pharmacokinetics, metabolism, excretion, and safety profile of the novel potassium-competitive acid blocker JP-1366 in humans to support its clinical development in China.
What are the pharmacokinetics, metabolism, and excretion of a single oral dose of [14C]JP-1366 in healthy Chinese male adults?
What are the pharmacokinetics, metabolism, and excretion of a single oral dose of [14C]JP-1366 in healthy Chinese male adults?
JP-1366 exhibits rapid absorption, extensive metabolism, and predominant fecal excretion in healthy Chinese adults, supporting its further clinical development.
Answers are grounded in this paper and cite their sources.
Supports dosing in Chinese patients; extends mass balance data to support further development but leaves clinical efficacy open.
Introduction JP-1366 (zastaprazan), a novel potassium-competitive acid blocker (P-CAB), was approved in South Korea in 2024 for treating erosive gastroesophageal reflux disease (GERD). This mass balance study characterized the pharmacokinetics, metabolism, excretion, and safety profile of JP-1366 in humans, supporting its further clinical development in China. Methods Six healthy Chinese male adults received a single oral dose of 20 mg (100 μCi) [ 14 C]JP-1366 under fasting conditions in this open-label Phase I study. Serial samples of blood, plasma, urine, and feces were collected and analyzed to determine Pharmacokinetic parameters, total radioactive recovery, metabolic fate, and excretion routes. Results JP-1366 was rapidly absorbed, with median T max values of 0.875 h observed for both the parent drug and total radioactivity in human plasma. The mean plasma elimination half-life (t 1/2 ) was approximately 28 h for JP-1366-related material. Furthermore, the blood-to-plasma ratio of total radioactivity ranged from 0.561 to 0.645, indicating limited distribution of drug-related material into blood cells. Within 264 h post-dose, 94.3% of the administered radioactive dose was recovered through excretion, predominantly via feces (51.9%) and urine (42.4%). JP-1366 underwent extensive metabolism in vivo , generating 57 metabolites, while the parent drug remained undetectable in excreted samples. The principal metabolic pathways involved oxidations (Phase I) and the following glucuronidation (Phase I/II). JP-1366 exhibited a favorable safety profile, with no serious adverse events reported. Conclusion JP-1366 exhibited favorable pharmacokinetic properties characterized by rapid absorption, extensive metabolism, and predominant fecal excretion of drug-related material. The principal metabolic pathways involved oxidations and the following glucuronidation. Clinical Trial Registration http://www.chinadrugtrials.org.cn/ , identifier CTR20244931.
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Liu et al. (2025) studied Healthy (n=6). [14C]JP-1366 was evaluated on Cumulative recovery of total radioactivity in excreta over 0-264 hours. [14C]JP-1366 was rapidly absorbed and extensively metabolized, with 94.3% of the administered radioactive dose recovered through excretion, predominantly via feces and urine.
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